Abstract
Aspalathin (2′,3,4,4′,6′-pentahydroxy-3′-C-β-D-glucopyranosyldihydrochalcone) is a natural C-linked glucosyl dihydrochalcone present in Aspalathus linearis (Burm.f.) R.Dahlgren (rooibos), a South African endemic plant, popularly consumed globally as a herbal tea. Aspalathin is reported to possess potent anti-oxidant properties that are believed to be responsible for the health benefits of rooibos. Other pharmacological properties ascribed to the molecule include antidiabetic, antimutagenic, anti-inflammatory, antithrombotic, and xanthine oxidase inhibitory activities. The role of aspalathin in limiting the progression of metabolic disorders and preventing diabetes-induced cardiovascular complications has been reported. The aforementioned potential health benefits of aspalathin have rendered it a popular natural ingredient that is incorporated in various nutraceutical and cosmeceutical products for protection against different conditions. Percutaneous permeation studies revealed some degree of absorption through the skin, supporting its use in cosmetic preparations. To perform an in-depth assessment of the scientific literature available on aspalathin, a bibliometric analysis was carried out on publications for the period 1965–2020, using the Scopus database. A total of 140 articles were retrieved, indicating that South African authors are major contributors to aspalathin research. The most common areas of investigation were identified as anti-oxidation, chemistry/chemical profiling, antidiabetic and anti-inflammatory activities. A comprehensive literature search showed that there are currently only two available reviews on aspalathin. Hence, the present review aims to explore the history and fill gaps with regards to collating aspects of the synthesis, quality control, metabolism and various biological activities of the molecule.
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Abbreviations
- A4:
-
Androstenedione
- 2-AAF:
-
2-Acetylaminofluorene
- ABTS:
-
2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)
- ACC:
-
Acetyl-CoA carboxylase
- ADP:
-
Adenosine diphosphate
- AFB1:
-
Aflatoxin B1
- AGE:
-
Advanced glycation end product
- AMPK:
-
Phosphorylation of AMP-activated protein kinase
- ATP:
-
Adenosine triphosphate
- AO:
-
Aortic output
- ARRE:
-
Aspalathin-rich rooibos extract
- Asp:
-
Aspalathin
- ATV:
-
Atorvastatin
- AUC:
-
Area under the curve
- BHA:
-
Butylated hydroxyanisole
- BHT:
-
Butylated hydroxytoluene
- BW:
-
Body weight
- CAMs:
-
Cell adhesion molecules
- CLP:
-
Cecal ligation puncture
- CPT1:
-
Carnitine palmitoyltransferase1
- DAD:
-
Diode array detection
- DCF:
-
2′,7′-Dichlorofluorescein diacetate
- ddY:
-
Deutschland, Denken, and Yoken
- DFT:
-
Density functional theory
- DMAP:
-
4-(Dimethylamino)pyridine
- DMF:
-
Dimethylformamide
- DNA:
-
Deoxyribonucleic acid
- Dox:
-
Doxorubicin
- DPPH:
-
2,2-Diphenyl-1-picrylhydrazyl
- DSS:
-
Dextran sodium sulfate
- EPCR:
-
Endothelial cell protein C receptor
- FAO:
-
Fatty acid β-oxidation
- FFA:
-
Free fatty acid
- FL:
-
Fluorescein
- FPG:
-
Fasting plasma glucose
- FRAP:
-
Ferric reducing antioxidant power
- FRE:
-
Fermented rooibos extract
- FT:
-
Fourier Transform
- G6Pase:
-
Glucose-6-phosphatase
- GAE:
-
Gallic acid equivalents
- GLUT:
-
Glucose transporter
- GP:
-
Glycogen phosphorylase
- GRE:
-
Green rooibos extract
- GRT:
-
Aspalathin-rich rooibos extract
- GS:
-
Glycogen synthase
- GSG:
-
Glutathione
- GSSG:
-
Oxidised glutathione
- HG:
-
High glucose
- hSGLT2:
-
Human sodium glucose co-transporter 2
- HPLC:
-
High-performance liquid chromatography
- HUVECs:
-
Human umbilical vein endothelial cells
- HW/BW:
-
Heart weight to body weight
- 11βOH-A4:
-
11-Hydroxyandrostenedione
- IC50 :
-
Half maximal inhibitory concentration
- IPGTT:
-
Intraperitoneal glucose tolerance test
- IRI:
-
Ischemia–reperfusion injury
- JC-1:
-
5,5′,6,6′-Tetrachloro-1,1′,3,3′-tetraethylimidacarbocyanine iodide
- LC–MS/MS:
-
Liquid chromatography-tandem mass spectrometry
- LPO:
-
Lipid hydroperoxide
- LPS:
-
Lipopolysaccharide
- LDL:
-
Low-density lipoprotein
- MBN:
-
Methylbenzylnitrosamine
- MDCK:
-
Madin-Darby canine kidney
- MRM:
-
Multiple reaction monitoring
- MTT:
-
3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide
- NADPH:
-
Nicotinamide adenine dinucleotide phosphate
- NG:
-
Normal glucose
- NIR:
-
Near infrared
- NMR:
-
Nuclear magnetic resonance
- Not:
-
Nothofagin
- ORAC:
-
Oxygen radical absorbance capacity
- pAMPK (Thr172):
-
Adenosine monophosphate-activated protein kinase threonine-172
- PI3K:
-
Phosphatidylinositol 3-kinase
- Papp:
-
Apparent rate of permeability
- PARP:
-
Poly (adenosine diphosphate ribose) polymerase
- PC:
-
Protein C
- PCR:
-
Polymerase chain reaction
- PEPK:
-
Phosphoenolpyruvate carboxykinase
- PgP:
-
P-glycoprotein
- PGR:
-
Pyrogallol red
- PPAG:
-
Phenylpyruvic acid-2-O-β-D-glucoside
- Rf:
-
Fermented rooibos aqueous extract
- RNA:
-
Ribonucleic acid
- ROS:
-
Reactive oxygen species
- SCD:
-
Stearoyl-coenzyme A desaturase
- scrRNA:
-
Scrambled ribonucleic acid
- SGLT:
-
Sodium glucose co-transporter
- siNrf2:
-
Small interfering nuclear factor erythroid 2-related factor 2
- SOD:
-
Superoxide dismutase
- STRING:
-
Search Tool for the Retrieval of Interacting Genes/Proteins
- STZ:
-
Streptozotocin
- TAC:
-
Total antioxidant capacity
- TE:
-
Trolox equivalent
- THF:
-
Tetrahydrofuran
- TLC:
-
Thin-layer chromatography
- UPLC-PDA:
-
Ultra performance liquid chromatography coupled to photodiode array detector
- TMSOTf:
-
Trimethylsilyl trifluoromethanesulfonate
- TPA:
-
12-O-Tetradecanoylphorbol-13-acetate
- UCP2:
-
Uncoupling protein 2
- XOD:
-
Xanthine oxidase inhibition
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The work was financially supported by the National Research Foundation of South Africa and the South African Medical Research Council.
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Chaudhary, S.K., Sandasi, M., Makolo, F. et al. Aspalathin: a rare dietary dihydrochalcone from Aspalathus linearis (rooibos tea). Phytochem Rev 20, 1161–1192 (2021). https://doi.org/10.1007/s11101-021-09741-9
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DOI: https://doi.org/10.1007/s11101-021-09741-9